Thorgeirsdóttir T O, Hilmarsson H, Thormar H, Kristmundsdóttir T
Faculty of Pharmacy, University of Iceland, Reykjavik, Iceland.
Pharmazie. 2005 Dec;60(12):897-9.
The lipid monocaprin (1-monoglyceride of capric acid) has been shown to be effective against enveloped viruses such as herpes simplex virus HSV in vitro. As it is known that HSV can develop resistance to acyclovir which is the most common treatment used, it was considered to be of interest to formulate a cream containing the lipid monocaprin as the active substance against HSV. The aim of this study was to develop an o/w-emulsion (cream) containing monocaprin and to evaluate the effects of formulation variables on the virucidal activity of monocaprin as well as the in vitro release rate of the monoglyceride from the formulations. The results show that release rate and extent of monocaprin release as well as the microbicidal properties of the the o/w-emulsion formulations are affected by the proportion of the oil phase and the amount of carbomer in the aqueous phase. Reducing the oil volume fraction increased antiviral effect and release of monocaprin from the formulation.
脂质单癸酸甘油酯(癸酸的1-单甘油酯)已被证明在体外对包膜病毒如单纯疱疹病毒(HSV)有效。由于已知HSV会对最常用的治疗药物阿昔洛韦产生耐药性,因此配制一种含有脂质单癸酸甘油酯作为抗HSV活性物质的乳膏被认为是有意义的。本研究的目的是开发一种含有单癸酸甘油酯的水包油乳液(乳膏),并评估配方变量对单癸酸甘油酯的杀病毒活性以及单甘油酯从配方中的体外释放速率的影响。结果表明,水包油乳液配方中,单癸酸甘油酯的释放速率和程度以及杀菌性能受油相比例和水相中卡波姆用量的影响。降低油相体积分数可增强抗病毒效果并促进单癸酸甘油酯从配方中的释放。